Compound name
SGC-AAK1-1
Protein family
Protein Kinase
Target name
AAK1
Affinity biochemical (nM)
9.1
Affinity on-target cellular (nM)
230
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000165b
SMILES
CCN(CC)S(=O)(=O)Nc1cccc(-c2ccc3c(NC(=O)C4CC4)n[nH]c3c2)c1
InChIKey
UCBIQZUJJSVQHL-UHFFFAOYSA-N
NCBI gene ID
22848
UniProt ID
Q2M2I8
Synonyms
KIAA1048, DKFZp686K16132
Mode of action
Inhibitor
Negative control
SGC-AAK1-1N
Affinity biochemical definition
Ki
Affinity biochemical assay type
TR-FRET binding-displacement assays
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acsmedchemlett.9b00399
https://www.thesgc.org/chemical-probes/SGC-AAK1-1
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (HEK293T cells)
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
403
Selectivity remarks
Screened at 1 µM, S(10) = 0.02, follow-up Kds for closest targets: Kd(PIP5K1C) = 260 nM, Kd(RIOK1) = 72 nM, Kd(RIOK3) = 290 nM; Kd(RIOK3) = 290 nM, Kd(CDKL2) = 880 nM, Kd(MYLK2) = 960 nM;
Selectivity Source Knowledge
https://doi.org/10.1021/acsmedchemlett.9b00399
https://www.thesgc.org/chemical-probes/SGC-AAK1-1
Selectivity Number of Off-targets
3